设计跨越蛋白类别的多配体的范例：双重 MCH-1R 拮抗剂/DPPIV 抑制剂。
An example of designed multiple ligands spanning protein classes: dual MCH-1R antagonists/DPPIV inhibitors.
机构信息
Prosidion Ltd, Windrush Court, Watlington Road, Oxford OX4 6LT, United Kingdom.
出版信息
Bioorg Med Chem Lett. 2012 Apr 1;22(7):2464-9. doi: 10.1016/j.bmcl.2012.02.010. Epub 2012 Feb 13.
PMID:22377519
Abstract
A ligand-based approach to identify potential starting points for a dual MCH-1R antagonist/DPPIV inhibitor medicinal chemistry program was undertaken. Potential ligand pairs were identified by analysis of MCH-1R and DPPIV in vitro data. A highly targeted synthetic effort lead to the discovery of pyridone 11, a dual MCH-1R antagonist/DPPIV inhibitor with selectivity over DPP8 and DPP9.
摘要
采用基于配体的方法，确定了潜在的双重 MCH-1R 拮抗剂/DPPIV 抑制剂药物化学项目的起始点。通过分析 MCH-1R 和 DPPIV 的体外数据，确定了潜在的配体对。经过高度靶向的合成努力，发现了吡啶酮 11，它是一种双重 MCH-1R 拮抗剂/DPPIV 抑制剂，对 DPP8 和 DPP9 具有选择性。
Zotero 插件